4-Methylumbelliferone (4-MU)

中文名称：4-甲基伞形酮

目录号：S2256 Purity: 99.89%

4-Methylumbelliferone (4-MU)是透明质酸(HA)合成抑制剂，IC50为0.4 mM。

4-Methylumbelliferone (4-MU) Chemical Structure

CAS: 90-33-5

规格	价格	库存
10mM (1mL in DMSO)	740.94	现货
10mg	563.57	现货
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产品质控

批次：纯度： 99.89%

99.89

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细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
HEK293T cells	Function assay	1 μM	24 hrs	Partial agonist activity at human PPARgamma-LBD expressed in HEK293T cells assessed as induction of receptor transactivation at 1 uM after 24 hrs by luciferase reporter gene assay	21030263
HepG2 cells	Function assay	10 umol/L	24 hrs	Increase in glucose consumption in human HepG2 cells at 10 umol/L after 24 hrs relative to control	21256748
Ac2F cells	Function assay	0.1 to 10 μM	6 hrs	Agonist activity at PPARgamma in rat Ac2F cells assessed as luciferase activity at 0.1 to 10 uM after 6 hrs by reporter gene assay	22819190
HepG2 cells	Function assay	10 uM	24 h	Reduction of glucose consumption in insulin-resistant human HepG2 cells at 10 uM after 24 hrs by glucose oxidase method in presence of 22.2 mM of glucose	23025244
HepG2 cells	Function assay	10 uM	24 h	Reduction of glucose consumption in insulin-resistant human HepG2 cells at 10 uM after 24 hrs by glucose oxidase method in presence of 0.1 uM of insulin	23025244
THP1 cells	Function assay	100 uM	3 hrs	Transactivation of PPARgamma in human THP1 cells assessed as decrease in LPS-induced MCP1 mRNA expression at 100 uM preincubated for 3 hrs prior to LPS challenge measured after 18 hrs by RT-PCR analysis relative to untreated control	22934537
THP1 cells	Function assay	100 uM	3 hrs	Transactivation of PPARgamma in human THP1 cells assessed as decrease in LPS-induced IL6 mRNA expression at 100 uM preincubated for 3 hrs prior to LPS challenge measured after 18 hrs by RT-PCR analysis relative to untreated control	22934537
HepaR cells	Function assay	1 uM	1 day	Agonist activity at PPARgamma in human HepaR cells assessed as increase in ANGPTL4 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control	25497132
HepaR cells	Function assay	1 uM	1 day	Agonist activity at PPARgamma in human HepaR cells assessed as increase in FABP1 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control	25497132
HEK293 cells	Function assay	10 μM	24 hrs	Transactivation of PPAR-gamma (unknown origin) expressed in HEK293 cells at 10 uM after 24 hrs by luciferase reporter gene assay	24890090
C2C12 cells	Function assay	30 μM	2 h	Induction of 2-deoxy-[3H]-glucose uptake in mouse C2C12 cells at 30 uM after 2 hrs by liquid scintillation counting analysis	25835537
HEK293 cells	Function assay	10 μM	24 h	Agonist activity at PPARgamma (unknown origin) expressed in HEK293 cells assessed as receptor transactivation at 10 uM incubated for 24 hrs by luciferase reporter gene assay	26384286
3T3L1 cell	Function assay	1 uM		Induction of mouse 3T3L1 cell differentiation assessed as increase in accumulation of intracellular lipid droplet at 1 uM by Oil red O staining	21401118
3T3L1 cells	Function assay	10 uM		Increase in adiponectin mRNA levels in TNFalpha-induced mouse 3T3L1 cells pretreated at 10 uM before TNF-alpha challenge relative to control	21851089
HEK293 cells	Function assay	10 μM		Transactivation of PPARgamma (unknown origin) expressed in HEK293 cells co-transfected with AP2-PPRE at 10 uM by luciferase reporter gene assay	23273519
3T3L1 cells	Function assay		7 days	Induction of adipogenesis in mouse 3T3L1 cells assessed as increase in lipid accumulation after 7 days by Oil red O staining	20527969
HEK293 cells	Function assay		16 to 20 hrs	Transactivation of Gal4-fused human PPARgamma expressed in HEK293 cells after 16 to 20 hrs by luciferase reporter gene assay, EC50=0.043 μM	21128600
CV1 cells	Function assay		40 h	Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay, EC50=0.1 μM	21515063
COS-1 cells	Function assay		24 hrs	Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis, EC50=0.048 μM	22051054
COS1 cells	Function assay		24 hrs	Transactivation of human full length PPARgamma expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay, EC50=0.12 μM	22197396
MG-63 cells	Function assay		24 hrs	Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assay, EC50=0.011 μM	22727448
293H DA cells	Function assay		16 h	Agonist activity at PPARgamma LBD in human 293H DA cells after 16 hrs by TR-FRET activation reporter assay, EC50=0.0024 μM	22582973
HepG2 cells	Function assay		20 h	Agonist activity at human GAL4-fused PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay, EC50=0.02 μM	22081932
HepG2 cells	Function assay		20 h	Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay, EC50=0.039 μM	23171045
HEK293 cells	Function assay		24 h	Transactivation of GAL4 DBD-fused human PPARgamma-LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay, EC50=0.1 μM	23294830
HEK293 cells	Function assay		48 hrs	Agonist activity at human PPARgamma expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay, EC50=43.71 μM	23265844
L6 cells	Function assay		24 hrs	Induction of glucose uptake in rat L6 cells pulsed with C14-deoxy glucose after 24 hrs in presence of insulin, EC50=4.49 μM	23992862
L6 cells	Function assay		16 hrs	Increase in 2-[3H]-deoxyglucose uptake in rat L6 cells after 16 hrs by scintillation counting analysis, EC50=4.8 μM	24813738
DU145 cells	Cytotoxicity assay		48 hrs	Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by MTT assay, EC50=16 μM	24996143
PC3 cells	Cytotoxicity assay		48 hrs	Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay, EC50=20.3 μM	24996143
MDA-MB-231 cells	Growth inhibition assay		24 hrs	Growth inhibition of human MDA-MB-231 cells after 24 hrs by MTT assay, EC50=5.23 μM	25278236
HepG2 cells	Function assay		20 hrs	Transactivation of PPAR transfected in human HepG2 cells after 20 hrs by PPAR-luciferase assay, EC50=1.6 μM	25437304
HEK293 cells	Function assay		24 hrs	Transactivation of PPARgamma (unknown origin) expressed in HEK293 cells incubated for 24 hrs by luciferase reporter gene assay	25442322
HEK293 cells	Function assay		24 hrs	Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay, EC50=0.03 μM	24955889
HepG2 cells	Function assay		20 hrs	Agonist activity at GAL4-DNA binding domain fused human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay, EC50=0.04 μM	25497132
HepaR cells	Function assay		1 day	Agonist activity at PPARgamma in human HepaR cells assessed as increase in HMGCS2 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control	25497132
MCF7 cells	Function assay		16 h	Agonist activity at human PPARgamma transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay, EC50=0.087 μM	26226490
COS1 cells	Function assay			Agonistic activity was determined in COS1 cells transfected with GAL 4-PPAR gamma receptor, EC50=0.021 μM	12617924
CV-1 cells	Function assay			Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay, EC50=0.043 μM	11720854
COS-1 cells	Function assay			In vitro transactivation of human peroxisome proliferator activated receptor gamma measured in PPAR-GAL4 chimeric COS-1 cells, EC50=0.02 μM	12873517
CV-1 cells	Function assay			Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells, EC50=0.08913 μM	9836620
CV-1 cells	Function assay			In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells, EC50=0.06 μM	8576907
COS-1 cells	Function assay			In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cells, EC50=0.02 μM	12729668
CV-1 cells	Function assay			In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined, EC50=0.325 μM	12954061
HepG2 cells	Function assay			Effective concentration against human PPARgamma expressed in HepG2 cells, EC50=0.039 μM	16107150
Huh7 cells	Function assay			Functional activity at human PPAR gamma in Huh7 cells by transactivation assay, EC50=0.22 μM	16366601
Huh7 cells	Function assay			Effect on PPAR gamma transactivation activity in Huh7 cells, EC50=0.22 μM	16451087
U2OS cells	Function assay			Effect on PPARgamma transactivation activity in U2OS cells, EC50=0.03 μM	16300944
CV1 cells	Function assay			Transactivation of PPARgamma in CV1 cells, EC50=0.076 μM	16821769
human keratinocytes	Proliferation assay			Antiproliferative activity against human keratinocytes, EC50=8 μM	16821769
HT29 cell	Proliferation assay			Antiproliferative activity against human HT29 cell line, EC50=45 μM	16821769
NIH3T3 cells	Function assay			Activity at human PPAR gamma transfected in NIH3T3 cells by luciferase activity assay, EC50=0.32 μM	16854085
CV1 cells	Function assay			Transactivation of human PPARgamma in CV1 cells by luciferase reporter gene assay, EC50=0.308 μM	16970391
Huh7 cells	Function assay			Activity at human PPAR gamma in Huh7 cells by transactivation assay, EC50=0.22 μM	17034149
HepG2 cells	Function assay			Agonist activity at human PPAR gamma in a HepG2 cells by PPAR-GAL4 transactivation assay, EC50=0.158 μM	16973358
HepG2 cells	Function assay			Agonist activity at human PPAR gamma in HepG2 cells by PPAR-GAL4 transactivation assay, EC50=0.158μM	16979341
CV1 cells	Function assay			Activity at human PPARgamma in CV1 cells, EC50=0.308 μM	17005394
HEK293 cells	Function assay			Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay, EC50=0.31 μM	17343371
rat L6 cells	Function assay			Effect on fatty acid oxidation in rat L6 cells, EC50=5 μM	17343371
HepG2 cells	Function assay			Agonist activity at human PPARgamma in HepG2 cells by PPAR-GAL4 transactivation assay, EC50=0.082 μM	17157019
CV1 cells	Function assay			Agonist activity at human PPARalpha in CV1 cells by GAL4 transactivation assay after 24 hrs, EC50=3.46 μM	17507225
CV1 cells	Function assay			Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs, EC50=0.03 μM	17507225
CV1 cells	Function assay			Agonist activity at human PPARgamma expressed in CV1 cells by receptor transactivation assay, EC50=0.308 μM	18029178
CV1 cells	Function assay			Agonist activity at PPARgamma in CV1 cells by transactivation assay, EC50=0.308 μM	17129725
HEK293 cells	Function assay			Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assay, EC50=0.035 μM	17292606
NIH3T3 cells	Function assay			Agonist activity at human PPARgamma expressed in NIH3T3 cells by GAL4 transactivation assay, EC50=0.32 μM	17624777
HEK293 cells	Function assay			Agonist activity at PPARgamma expressed in HEK293 cells by GAL4 transactivation assay, EC50=0.19 μM	18029176
HEK293 cells	Function assay			Agonist activity at PPARgamma expressed in HEK293 cells assessed as aP2 gene induction, EC50=0.12 μM	18029176
HEK293 cells	Function assay			Agonist activity at PPARgamma in HEK293 cells by GAL4 transactivation assay, EC50=0.045 μM	18291645
HepG2 cells	Function assay			Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay, EC50=0.039 μM	18835719
RAW264.7 cells	Function assay			Suppression of LPS/IFN-gamma-stimulated NO production in mouse RAW264.7 cells, EC50=17.5 μM	18809325
BL21 cells	Function assay			Displacement of radio labeled 2(S)-(2-benzoyl-phenylamino)-3-{4-[1,1-ditritio-2-(5-methyl-2-phenyl-oxazol-4-yl)-ethoxy]-phenyl}-propionic acid from GST-fused human PPARgamma expressed in Escherichia coli BL21 cells by scintillation proximity assay, EC50=0.45 μM	19349176
BHK21 cells	Function assay			Agonist activity at human PPARgamma expressed in BHK21 cells assessed as SEAP activity by luciferase reporter transactivation assay, EC50=0.45 μM	19349176
HepG2/C3A cells	Function assay			Activation of human PPARgamma ligand binding domain-mediated transcriptional activity in human HepG2/C3A cells co-transfected with fused Gal4-LBD by cotransfection assay, EC50=0.0038 μM	17403688
HepG2 cells	Function assay			Agonist activity at PPARgamma expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control, EC50=0.05 μM	18625559
COS1 cells	Function assay			Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by luciferase reporter gene assay, EC50=0.02 μM	19507861
HepG2 cells	Function assay			Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay, EC50=0.223 μM	18394907
CV1 cells	Function assay			Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50=0.033 μM	18826205
CV1 cells	Function assay			Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50=3.46 μM	18826205
U2OS cells	Function assay			Agonist activity at human PPARgamma in U2OS cells by transactivation assay, EC50=0.02 μM	18329751
Hep G2 cells	Function assay			Agonist activity at human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay, EC50=0.04 μM	19053776
HeLa cells	Function assay			Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay, EC50=0.015 μM	19275963
COS1 cells	Function assay			Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay, EC50=0.02 μM	19530681
U2OS cells	Function assay			Agonist activity at human PPARgamma expressed in U2OS cells by luciferase transactivation assay, EC50=0.05 μM	19574056
HepG2 cells	Function assay			Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay, EC50=0.039 μM	19775169
HepG2 cells	Function assay			Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay, EC50=0.223 μM	19783444
COS7 cells	Function assay			Agonist activity at human recombinant PPARgamma2 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay, EC50=0.1 μM	20138762
COS7 cells	Function assay			Agonist activity at human recombinant PPARgamma1 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay, EC50=0.03 μM	20138762
HEK cells	Function assay			Agonist activity at human GAL4-tagged PPARalpha chimeric receptor expressed in HEK cells by transactivation assay, EC50=10.58 μM	20299214
HEK cells	Function assay			Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assay, EC50=0.035 μM	20299214
CHO-K1 cells	Function assay			Partial agonist activity at human PPARgamma-LBD expressed in CHO-K1 cells co-transfected with GAL4 assessed as luciferase activity by transactivation assay, EC50=0.1 μM	20527969
CV1 cells	Function assay			Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay, EC50=0.1 μM	21112784
HepG2 cells	Function assay			Agonist activity at PPARgamma receptor expressed in human HepG2 cells by PPRE-luciferase reporter gene assay, EC50=0.01 μM	21482446
HepG2 cells	Function assay			Transactivation of human PPARgamma expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay, EC50=0.05 μM	21450468
COS7 cells	Function assay			Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay, EC50=0.043 μM	21873070
MG-63 cells	Function assay			Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assay, EC50=0.011 μM	22225641
COS1 cells	Function assay			Binding affinity to human wild type PPARgamma LBD expressed in COS1 cells co-expressing GAL4 by scintillation proximity assay	22070604
HepG2 cells	Function assay			Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells by luciferase reporter gene assay, EC50=0.1 μM	22934537
BL21 DE3 cells	Function assay			Displacement of [3H]rosiglitazone from N-terminal His-tagged human PPARgamma ligand binding domain expressed in Escherichia coli BL21 DE3 cells by scintillation proximity assay, Ki=0.074 μM	22081932
human L02 cells	Function assay			Agonist activity at PPARgamma-LBD expressed in human L02 cells co-expressing pGL3-SV40-GAL4 after 24 hrs by luciferase reporter gene based transactivation assay, EC50=0.9 μM	23186307
HEK293 cells	Function assay			Agonist at human PPARgamma LBD expressed in human HEK293 cells cotransfected with GAL4-Luc assessed as transcriptional activation by luciferase reporter gene assay, EC50=0.004 μM	23286787
HepG2 cells	Function assay			Agonist activity at GAL4-fused PPARgamma (unknown origin) expressed in human HepG2 cells by transactivation assay, EC50=0.01 μM	23502212
HepG2 cells	Function assay			Agonist activity at GAL4-fused PPARgamma M463A mutant (unknown origin) expressed in human HepG2 cells by transactivation assay, EC50=0.002 μM	23502212
HEK293 cells	Function assay			Agonist activity at human PPARgamma expressed in HEK293 cells by luciferase reporter gene assay, EC50=0.01 μM	25305688
HepG2 cells	Function assay			Agonist activity at human GAL4-PPARgamma ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay, EC50=0.039 μM	25462281
点击查看更多细胞系数据

生物活性

产品描述	4-Methylumbelliferone (4-MU)是透明质酸(HA)合成抑制剂，IC50为0.4 mM。

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05295680	Recruiting	Primary Sclerosing Cholangitis	Aparna Goel\|Stanford University	May 10 2023	Phase 2

化学信息&溶解度

分子量	176.17	分子式	C₁₀H₈O₃
CAS号	90-33-5	SDF	Download 4-Methylumbelliferone (4-MU) SDF
Smiles	CC1=CC(=O)OC2=C1C=CC(=C2)O
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 35 mg/mL ( (198.67 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 35 mg/mL (198.67 mM)

Water : Insoluble

DMSO : 35 mg/mL ( (198.67 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 35 mg/mL (198.67 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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如果有其他问题，请给我们留言。

* 必填项

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):